AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesGeographicals
ChloroquineAntimalarialsDrug ResistancePlasmodium falciparumParasitic Sensitivity TestsMalaria, FalciparumPrimaquinePyrimethamineSulfadoxineMefloquineProtozoan ProteinsMalariaQuinineDrug CombinationsAmodiaquineMalaria, VivaxMembrane Transport ProteinsArtemisininsPlasmodium vivaxParasitemiaProguanilAmmonium ChlorideInhibitory Concentration 50LysosomesPlasmodium bergheiSesquiterpenesFluorenesDNA, ProtozoanIndonesiaAminoquinolinesHydroxychloroquineDrug Therapy, CombinationCameroonQuinolinesSenegalPromethazineMonensinPheniramine
PlasmodiumPhosphateMalariaHydroxychloroquineQuinineParasitesVitroArtemisinin-based combinationCimetidineIsolatesInhibitoryRetinopathyPfCRTVerapamilHemozoinMechanism of ActDiphosphateStrainsAntiviralSulfadoxineTherapeuticHemeAralenDegradationDosesCompoundDrugsExcretionRapidlyInfectionReplicationVivoTreatmentToxicDosageDoseAntibioticsHemoglobinPlasma concentrationUrineLupusDigestiveTissuesDecreasesTabletHighAcidicPump
Plasmodium14
Phosphate11
Malaria11
  • Chloroquine (CQ), a 4-aminoquinoline, accumulates in acidic digestive vacuoles of the malaria parasite, preventing conversion of toxic haematin to beta-haematin. (nih.gov)
  • Hydroxychloroquine and chloroquine are used extensively in malaria and rheumatological conditions, and now in COVID-19 prevention and treatment. (ox.ac.uk)
  • In these tests, blood samples from malaria patients are cultured and if found to be viable, the malaria parasites are exposed to different concentrations of antimalarial drugs in the laboratory. (cdc.gov)
  • Chloroquine is a synthetic drug mainly used for the treatment of malaria. (vedantu.com)
  • ABSTRACT Pregnant Sudanese women who presented at a hospital in eastern Sudan with chloroquine- resistant falciparum malaria were randomly allocated to one of two quinine regimens: low-dose (10 mg/kg 2 times/day) (18 patients) or standard (10 mg/kg 3 times/day) (24 patients). (who.int)
  • Quinine is the treatment of choice for se- and obstetric history, physical examination vere and chloroquine-resistant falciparum and use of antimalarials in the 3 weeks be- malaria. (who.int)
  • BACKGROUND: The predominance of chloroquine-susceptible falciparum malaria in Malawi more than a decade after chloroquine's withdrawal permits contemplation of re-introducing chloroquine for targeted uses. (emmes.com)
  • Participants were randomized to receive chloroquine alone or combined with artesunate, azithromycin or atovaquone-proguanil for all episodes of uncomplicated malaria for one year. (emmes.com)
  • Malaria incidence (95% confidence interval) was 0.59 (.46-.74), .61 (.49-.76), .63 (.50-.79) and .68 (.54-.86) episodes/person-year for group randomized to receive chloroquine alone or in combination with artesunate, azithromycin or atovaquone-proguanil respectively and the differences were not statistically significant. (emmes.com)
  • Treatment efficacy for first episodes was 100% for chloroquine monotherapy and 97.9% for subsequent episodes of malaria. (emmes.com)
  • As such, chloroquine is the archetypal antiparasitic treatment for malaria. (pixorize.com)
Hydroxychloroquine6
Quinine6
  • We tested antimalarials that are currently in use in this country (chloroquine, amodiaquine, quinine, and pyrimethamine), antimalarials that will become available in this region in the future (artemisinin and halofantrine), and prophylactic antimalarials (mefloquine, doxycycline, and atovaquone). (pasteur.fr)
  • The proportions of resistant isolates were 37% for chloroquine, 15.9% for amodiaquine, 0% for quinine, 0% for dihydroartemisinin, 1.6% for mefloquine, 3.8% for halofantrine, 4.0% for atovaquone, and 38.3% for pyrimethamine. (pasteur.fr)
  • Criteria for defining more-reliable IC50s based on estimated confidence intervals and growth ratios improved correlation coefficients for the drug pairs mefloquine-quinine and chloroquine-desethylamodiaquine in 9 of 11 and 8 of 8 data sets, respectively. (wwarn.org)
  • The in vivo and in vitro susceptibilities to quinine and quinidine, compared to chloroquine, were studied by investigating the number of treatment days required for radical cure and estimating the quinine concentrations concomitantly. (bvsalud.org)
  • The minimal inhibitory concentrations (MIC) for schizont maturation in all successful in vitro tests were 5.12 x 10(-6) mol/l for quinine and 1.28 x 10(-6) mol/l for quinidine, indicating that all 50 isolates were sensitive to the two drugs. (bvsalud.org)
  • The IC50, IC90 and geometrical mean MIC for quinine were all about two times higher for the chloroquine-resistant than for the chloroquine-sensitive isolates (P = 0.006). (bvsalud.org)
Parasites8
  • The resistant parasites use its transmembrane pump to remove chloroquine from the digestive vacuole. (vedantu.com)
  • These chloroquine-resistant parasites pump out 40 times more than the chloroquine-sensitive parasites. (vedantu.com)
  • A Ca²⁺ channel blocker Verapamil has found to restore the ability of chloroquine to treat resistance parasites. (vedantu.com)
  • Resistance to chloroquine occurs through drug efflux, which reduces the levels of the drug inside parasites. (pixorize.com)
  • The very fast efflux of the pre-accumulated drug from chloroquine-resistant (CQR) parasites resulted in a differential in the drug retained by resistant and sensitive parasites. (elsevierpure.com)
  • The chloroquine-sensitive parasites retained 2-3 times more chloroquine than resistant parasites. (elsevierpure.com)
  • This confirmed the suggestion that verapamil inhibits the rapid efflux in CQR parasites resulting in a readily detectable increase in chloroquine accumulation. (elsevierpure.com)
  • In vitro inhibition of parasites by 1.6 x 10(-6) mol/l of chloroquine was obtained in 31 out of 47 isolates, 16 (34%) being resistant. (bvsalud.org)
Vitro6
  • Chloroquine inhibited virus replication in vitro, but only at cytotoxic concentrations. (cdc.gov)
  • Previous in vitro data state a half maximal effective concentration (EC 50 ) and EC 90 of 16 and 25 mol/L for chloroquine against Ebola virus (EBOV), respectively ( 8 ). (cdc.gov)
  • To determine whether protection would extend to the EBOV hamster model, during 2013-2014 we investigated chloroquine treatment in this model and attempted to repeat previous in vitro findings and findings in the mouse model. (cdc.gov)
  • In-vitro data suggest that high concentrations and thus high doses are needed for COVID-19 infections, but as yet there is no convincing evidence of clinical efficacy. (ox.ac.uk)
  • In vitro studies with trophozoites of Entamoeba histolytica have demonstrated that chloroquine also possesses amebicidal activity comparable to that of emetine. (drugs.com)
  • Analysis of the key pfcrt point mutation and in vitro and in vivo response to chloroquine in Yaounde, Cameroon. (ajtmh.org)
Artemisinin-based combination1
  • We included studies if they had active follow-up of at least 28 days, and if they included a treatment group with daily primaquine given over multiple days, where primaquine was commenced within 7 days of schizontocidal treatment and was given alone or coadministered with chloroquine or one of four artemisinin-based combination therapies (ie, artemether-lumefantrine, artesunate-mefloquine, artesunate-amodiaquine, or dihydroartemisinin-piperaquine). (cdc.gov)
Cimetidine2
  • Ali, BH, Al-Qarawi, A & Mousa, HM 2001, ' Effect of grapefruit juice and cimetidine on the concentration of chloroquine in plasma of chickens ', Indian Journal of Pharmacology , المجلد 33, رقم 4, الصفحات 289-290. (elsevierpure.com)
  • Mousa, H. M. / Effect of grapefruit juice and cimetidine on the concentration of chloroquine in plasma of chickens . (elsevierpure.com)
Isolates1
  • Drug concentrations associated with half-maximal inhibition of growth (IC50s) were determined by a modified sigmoid Emax model-fitting algorithm, allowing standardized analysis of 7,350 concentration-inhibition assays involving 1,592 isolates. (wwarn.org)
Inhibitory1
  • The mean 50% inhibitory concentration ( IC 50 ) for Artemotil is 1.61 nM (range 1.57-1.92 nM). (medchemexpress.com)
Retinopathy2
PfCRT2
  • P. falciparum codes the pump by the chloroquine resistance transporter (PfCRT) gene. (vedantu.com)
  • Secondary endpoints included treatment efficacy, and incidence of the chloroquine resistance marker pfcrt T76 and of anemia. (emmes.com)
Verapamil5
  • To evaluate effects on autophagy, cells were treated with various concentrations of chloroquine or verapamil for 48 h. (moleculardevices.com)
  • Verapamil induces autophagy while chloroquine inhibits degradation of autophagosomes that lead to accumulation of particles. (moleculardevices.com)
  • Concentration responses for chloroquine and verapamil were examined and EC 50 values were evaluated. (moleculardevices.com)
  • Chloroquine and verapamil treatment increased autophagy levels by 4.6 and 3.3-fold, respectively, as determined by total autophagosome counts (EC 50 values were 4.0 and 3.6 μM respectively). (moleculardevices.com)
  • The steady-state uptake of [ 3 H]chloroquine appeared to be enhanced by verapamil and desipramine in the chloroquine-resistant clones, while the opposite was observed with sensitive clones. (elsevierpure.com)
Hemozoin2
  • Chloroquine covers hemozoin molecules to prevent further biocrystallization of heme thus helps to heme buildup. (vedantu.com)
  • If the parasite does not form hemozoin, then it is resistant to chloroquine. (vedantu.com)
Mechanism of Act1
Diphosphate1
  • Effect of high vs low doses of chloroquine diphosphate as adjunctive therapy for patients hospitalized with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection: a randomized clinical trial, JAMA Netw. (c19hcq.org)
Strains5
  • This conclusion implies that chloroquine functions both as a preventative vaccine and as a cure for strains of coronavirus. (waccobb.net)
  • P. falciparum is a resistant strains of chloroquine. (vedantu.com)
  • These strains are showing resistant behaviour to chloroquine this is because mainly due to the evolution of species. (vedantu.com)
  • CS and CR are chloroquine-sensitive and -resistant strains respectively. (biomedcentral.com)
  • After that antimalarial activities of the extracts were evaluated against both chloroquine sensitive (3D7) and resistant (RKL-9) strains of P. falciparum using Giemsa staining light microscopy technique. (springeropen.com)
Antiviral2
Sulfadoxine2
  • For some drugs (chloroquine, sulfadoxine-pyrimethamine and similar drugs, atovaquone), molecular markers have been identified that confer resistance. (cdc.gov)
  • It also reviews the way drug resistance develops and spreads, methods used to assess the presence and level of drug resistance, and the extent to which chloroquine and sulfadoxine/pyrimethamine (SP)-the two most widely used antimalarial drugs in the world today-have now lost efficacy. (nationalacademies.org)
Therapeutic3
  • This effect may underlie therapeutic efficiency of chloroquine known to act as zinc ionophore. (spandidos-publications.com)
  • High plasma concentration and maximum therapeutic effect is achieved within one to six hours. (edexpress24.net)
  • Chloroquine metabolites have therapeutic activity and are primarily excreted by kidneys. (edexpress24.net)
Heme2
  • The chloroquine join to heme to form the FP-chloroquine complex. (vedantu.com)
  • Chloroquine is an antiparasitic drug that blocks the breakdown of heme, causing an accumulation of heme. (pixorize.com)
Aralen1
  • Chloroquine is the active substance, based on which the original drug Aralen was created. (edexpress24.net)
Degradation1
  • Chloroquine undergoes appreciable degradation in the body. (drugs.com)
Doses1
  • Bayesian regression models were fitted to survival outcomes and electrocardiograph QRS durations from 302 prospectively studied French patients who had taken intentional chloroquine overdoses, of whom 33 died (11%), and 16 healthy volunteers who took 620 mg base chloroquine single doses. (ox.ac.uk)
Compound2
  • At a free drug concentration of 0.1 mM, binding ranged between 0.8 nmol/mg for pirenzepine and 71 nmol/mg for chloroquine, a compound which has been described as provoking toxic side-effects in melanin-containing tissues and adjacent structures. (aspetjournals.org)
  • The EC 50 is the IC 50 of the isolated compound and "x" is the yield-dependent calculated concentration of the compound at the IC 50 of the extract. (biomedcentral.com)
Drugs3
  • We aimed to compare the ability of different partner drugs to preserve chloroquine efficacy and prevent the re-emergence of resistance. (emmes.com)
  • Overall, these findings confirm the fixation of chloroquine and pyrimethamine-resistant alleles already described in the literature, implying that these drugs are not currently appropriate for use in Colombia. (biomedcentral.com)
  • Examination of concentration-inhibition data revealed evidence of apparent paradoxical growth at high concentrations of nonartemisinin drugs, supporting amendment of the method for calculating the maximal drug effect in each assay. (wwarn.org)
Excretion1
Rapidly3
  • Twice daily dosing at 90 mg/kg intraperitoneally rapidly achieved a steady-state concentration of 2.5 μg/mL in the blood of mice. (cdc.gov)
  • Chloroquine is rapidly and almost completely absorbed from the gastrointestinal tract, and only a small proportion of the administered dose is found in the stools. (drugs.com)
  • However, under an atmosphere of air the chloroquine-resistant P. falciparum clones released pre-accumulated [ 3 H]chloroquine more rapidly than sensitive clones. (elsevierpure.com)
Infection3
  • The antimalarial drug chloroquine has been suggested as a treatment for Ebola virus infection. (cdc.gov)
  • These data have led to the suggestion that chloroquine and its derivatives be used in persons with EBOV infection because this drug is approved for use in humans, has an extensive safety profile, and is inexpensive ( 1 , 9 ). (cdc.gov)
  • When added 1 h after infection, chloroquine at 5 μg/mL and 25 μg/mL reduced the viral loads by 0.61 and 1.07 logs, respectively (peak reduction observed on day 5), without any significant cytotoxicity ( Figure 1 ). (cdc.gov)
Replication1
  • As we've written before , research indicates that high concentrations of zinc inside cells inhibit the replication of RNA viruses such as COVID-19, but due to zinc's other characteristics, cells do not typically tolerate high levels of this mineral. (anh-usa.org)
Vivo1
  • In vivo antiplasmodial studies with P. falciparum infected mice showed an effect of 4,7-dichloroquinoline compared to chloroquine. (nature.com)
Treatment3
  • Chloroquine is not a promising treatment for Ebola. (cdc.gov)
  • Treatment groups (mice and hamsters) received 90 mg/kg of chloroquine alone (intraperitoneally). (cdc.gov)
  • CONCLUSION/SIGNIFICANCE: Sustained chloroquine efficacy with repeated treatment supports the eventual re-introduction of chloroquine combinations for targeted uses such as intermittent preventive treatment. (emmes.com)
Toxic1
  • The action of the toxic FP and FP- chloroquine results in cell lysis and supports parasite cell autodigestion. (vedantu.com)
Dosage1
  • The kinetics of chloroquine metabolism are complex, with the half-life increasing with increasing dosage. (medscape.com)
Dose1
  • Volume of distribution provides a reference for the plasma concentration expected for a given dose but provides little information about the specific pattern of distribution. (msdmanuals.com)
Antibiotics1
  • This chloroquine will interact with other medications namely, antibiotics like ampicillin, erythromycin, antacids, antiarrhythmics which increases side effects. (vedantu.com)
Hemoglobin1
  • Young children treated with chloroquine-azithromycin had higher hemoglobin concentrations at the study's end than did those in the chloroquine monotherapy group. (emmes.com)
Plasma concentration2
  • After equilibrium, drug concentrations in tissues and in extracellular fluids are reflected by the plasma concentration. (msdmanuals.com)
  • thus, plasma concentration is low and volume of distribution is high. (msdmanuals.com)
Urine1
  • Urine color varies based on the urine concentration and chemical composition. (medscape.com)
Lupus1
  • Another scholarly research uncovered Propofol that previous BWF1 mice, when contaminated with on the starting point of clinical signals of lupus and eventually treated with Eltd1 chloroquine, created temporary remission from the symptoms. (findadig.com)
Digestive1
  • Chloroquine transfers CQ2+ protons as the digestive vacuole is acidic. (vedantu.com)
Tissues1
  • Chloroquine is deposited in the tissues in considerable amounts. (drugs.com)
Decreases1
  • The antibiotic rifampicin decreases plasma concentrations of praziquantel. (wikipedia.org)
Tablet1
  • Chloroquine tablet uses brings some side effects. (vedantu.com)
High2
  • The drug is extracted from the blood and the concentration is determined by high-performance liquid chromatographic methods. (cdc.gov)
  • In summary, our results demonstrate that A549 cells are insensitive to both low and high concentrations of green tea extract, likely due to the induction of cytoprotective autophagy. (bioinformation.net)
Acidic1
  • Chloroquine drug concentrates on acidic food vacuole of the parasite and enters into the essential process. (vedantu.com)
Pump1